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著者

九州大学大学院薬学研究科Graduate School of Pharmaceutical Sciences, Kyushu University

抄録

Since the discovery of morphine-6-glucuronide over three decades ago, an increasing body of work has emerged supporting the concept of an active metabolite in experimental animals and humans. Pharmacological characterization with antisense oligodeoxynucleotide of mu-opioid receptor, MOR-1 and receptor binding study have suggested the existence of an unique receptor of mu-subtype for morphine-6-glucuronide. In this review, our studies on species difference of site selective glucuronidation of morphine and UDP-glucuronosyltransferases responsible for the glucuronidation were presented. Recent experimental evidence supporting the view that UDP-glucuronosyltransferase isoforms could act as hetero-oligomers by accessing a broader range of substrates is included.